Name of the medicinal product
Vastarel MR, modified release film-coated tablets in 10's and 60's / box.
Qualitative and quantitative composition
Trimetazidine dihydrochloride 35 mg
Excipients q.s. for one modified release
• Pharmacodynamic properties
Other cardiovascular antianginal drug Code ATC: C01EB15
(C: cardiovascular system)
By preserving energy metabolism in cells exposed to hypoxia or ischaemia,
trimetazidine prevents a decrease in intracellular ATP levels, thereby
ensuring the proper functioning of ionic pumps and transmembrane
sodium-potassium flow whilst maintaining cellular homeostasis.
helps maintain energy metabolism in the heart and neurosensory organs during
episodes of ischaemia and hypoxia,
reduces intracellular acidosis and alterations in transmembrane ion flow
caused by ischaemia,
decreases the migration and infiltration of polynuclear neutrophils in
ischaemic and reperfused cardiac tissue. It also reduces the size of
- exerts this action in the absence of any direct haemodynamic effect.
Controlled studies in angina patients have
shown that trimetazidine:
increases coronary flow reserve, thereby delaying the onset of
exercise-induced ischaemia, starting from the 15th day of treatment,
limits rapid swings in blood pressure without any significant variations in
- significantly decreases the frequency of angina attacks,
leads to a significant decrease in the use of trinitroglycerin.
In a two-month study in patients receiving 50 mg atenolol, adding one 35 mg
trimetazidine modified release tablet produced a significant increase in the
time to 1-mm ST-segment depression in exercise tests, when compared to a
placebo, 12 hours after taking the drug.
• Pharmacokinetic properties
- After oral administration, maximum
concentration is found, on average, 5 hours after taking the tablet. Over 24
hours the plasma concentration remains at levels above or equal to 75% of
the maximum concentration for 11 hours.
Steady state is reached by the 60th
hour, at the latest.
The pharmacokinetic characteristics of Vastarel MR are not influenced by
The apparent distribution volume is 4.8 I/kg; protein binding is low: in
vitro measurements give value of 16%.
Trimetazidine is eliminated primarily in the urine, mainly in the unchanged
form. The elimination half-life of Vastarel MR is an
average of 7 hours in healthy young volunteers and 12 hours in subjects aged
more than 65 years. Total clearance of trimetazidine is the result of major
renal clearance which is directly correlated to creatinine clearance and, to
a lesser extent, to liver clearance which is reduced with age.
- A specific clinical study carried out in an elderly population using a
dosage of 2 tablets per day taken in 2 doses, analysed by a kinetic
population method, showed an increase in plasma exposure which does not
justify a dosage alteration.
Prophylactic treatment of episodes of angina pectoris.
Adjuvant symptomatic treatment of vertigo and tinnitus.
Adjuvant treatment of the decline in visual acuity and visual field
disturbances presumably of vascular origin.
Hypersensitivity to the active substance or to any of the excipients.
The use of this medicinal product is not recommended during pregnancy and
breast-feeding (see section Pregnancy and lactation)
Special warnings and precautions for use
This drug is not a curative
treatment for angina attacks, nor is it indicated as an initial treatment
for unstable angina, or myocardial infarction. In the event of an angina
attack, the coronaropathy should be reevaluated and an adaptation of the
treatment considered (drug treatment and possibly revascularisation).
Pregnancy & breast-feeding
No teratogenic effect was seen in animal studies; in the absence of clinical
data, a risk of birth defect induction cannot be excluded;
consequently, as a precaution, it is best not to prescribe the drug during
In the absence of data on excretion of the drug in milk, breast-feeding is
not recommended during treatment.
Rare cases of gastrointestinal disorders (nausea and vomiting).
Interaction with other medicinal products and other forms of interaction
No drug interaction has been reported; in particular, trimetazidine can be
prescribed in combination with heparin, calciparin, vitamin K antagonist,
oral hypolipidaemia agents, aspirin, beta-blockers, calcium inhibitors,
digitalis (Trimetazidine has no effect on the plasma levels of digoxin).
Dosage and method of administration
One tablet at mealtimes in the morning and evening.
The experience of overdosage is very limited. Patients should be monitored
in terms of cardiovascular and hemodynamic parameters.
No special storage condition required. Store below 30°C.